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TWI462915B - 一種組織胺h3受體拮抗劑的新穎富馬酸鹽 - Google Patents

一種組織胺h3受體拮抗劑的新穎富馬酸鹽 Download PDF

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Publication number
TWI462915B
TWI462915B TW099120734A TW99120734A TWI462915B TW I462915 B TWI462915 B TW I462915B TW 099120734 A TW099120734 A TW 099120734A TW 99120734 A TW99120734 A TW 99120734A TW I462915 B TWI462915 B TW I462915B
Authority
TW
Taiwan
Prior art keywords
ethyl
cyclohexylmethyl
sulfonamide
methyl
pyrrolidin
Prior art date
Application number
TW099120734A
Other languages
English (en)
Chinese (zh)
Other versions
TW201103911A (en
Inventor
Beverly C Langevin
Robert Allan Farr
Dinubhai H Shah
Daniel Sherer
Original Assignee
Sanofi Aventis
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Filing date
Publication date
Application filed by Sanofi Aventis filed Critical Sanofi Aventis
Publication of TW201103911A publication Critical patent/TW201103911A/zh
Application granted granted Critical
Publication of TWI462915B publication Critical patent/TWI462915B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Anesthesiology (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW099120734A 2009-06-26 2010-06-25 一種組織胺h3受體拮抗劑的新穎富馬酸鹽 TWI462915B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22068309P 2009-06-26 2009-06-26
FR0959110 2009-12-17

Publications (2)

Publication Number Publication Date
TW201103911A TW201103911A (en) 2011-02-01
TWI462915B true TWI462915B (zh) 2014-12-01

Family

ID=43386878

Family Applications (1)

Application Number Title Priority Date Filing Date
TW099120734A TWI462915B (zh) 2009-06-26 2010-06-25 一種組織胺h3受體拮抗劑的新穎富馬酸鹽

Country Status (25)

Country Link
US (1) US8664245B2 (fr)
EP (1) EP2445899B1 (fr)
JP (1) JP6053519B2 (fr)
KR (1) KR101804749B1 (fr)
CN (1) CN102803247B (fr)
AR (1) AR077223A1 (fr)
AU (1) AU2010264422B2 (fr)
BR (1) BRPI1011258A2 (fr)
CA (1) CA2766154C (fr)
CO (1) CO6480943A2 (fr)
DO (1) DOP2011000398A (fr)
ES (1) ES2587064T3 (fr)
IL (1) IL216924A0 (fr)
MA (1) MA33378B1 (fr)
MX (1) MX2011012824A (fr)
NZ (1) NZ597219A (fr)
PE (1) PE20121403A1 (fr)
PL (1) PL2445899T3 (fr)
RU (1) RU2537847C2 (fr)
SG (1) SG176645A1 (fr)
TN (1) TN2011000620A1 (fr)
TW (1) TWI462915B (fr)
UY (1) UY32738A (fr)
WO (1) WO2010151611A1 (fr)
ZA (1) ZA201108838B (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR080374A1 (es) 2010-03-05 2012-04-04 Sanofi Aventis Procedimiento para la preparcion de 2-(ciclohexilmetil)-n-(2-((2s)-1-metilpirrolidin-2-il) etil)- 1,2,3,4-tetrahidroisoquinolin-7- sulfonamida
WO2013151982A1 (fr) 2012-04-03 2013-10-10 Arena Pharmaceuticals, Inc. Méthodes et composés utiles pour traiter le prurit, et procédés d'identification desdits composés
EP2647377A1 (fr) * 2012-04-06 2013-10-09 Sanofi Utilisation d'un antagoniste du récepteur h3 pour le traitement de la maladie d'Alzheimer
JP2015524400A (ja) * 2012-07-19 2015-08-24 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 9−[4−(3−クロロ−2−フルオロ−フェニルアミノ)−7−メトキシ−キナゾリン−6−イルオキシ]−1,4−ジアザ−スピロ[5.5]ウンデカン−5−オンのフマル酸塩、その薬物としての使用及び調製
WO2015032966A1 (fr) * 2013-09-09 2015-03-12 Sanofi Antagoniste des récepteurs h3 combiné à un inhibiteur de la cholinestérase et utilisé dans le cadre du traitement de la maladie d'alzheimer

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070105834A1 (en) * 2004-05-25 2007-05-10 Sanofi-Aventis Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics
US20080318952A1 (en) * 2007-05-18 2008-12-25 Keith John M Diaryl-substituted tetrahydroisoquinolines as histamine h3 receptor and serotonin transporter modulators

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4228170A (en) 1979-08-30 1980-10-14 Smithkline Corporation 7- and/or 8-Sulfur substituted 1,2,3,4-tetrahydroisoquinoline compounds
EP0306375A1 (fr) 1987-08-07 1989-03-08 Synthelabo Dérivés de[(pipéridinyl-4)méthyl]-2 tétrahydro-1,2,3,4 isoquinoléine, leur préparation et leur application en thérapeutique
IL89156A (en) 1988-07-12 1993-05-13 Synthelabo Derivatives of 2-((4-piperidinyl) methyl)- 1,2,3,4- tetrahydroisoquinoline, their preparation and their application in therapeutics
SK1212002A3 (en) 1999-07-29 2002-11-06 Egyt Gyogyszervegyeszeti Gyar Isoquinoline derivatives, pharmaceutical compositions containing the same, and a process for the preparation of the active substance
US6825198B2 (en) * 2001-06-21 2004-11-30 Pfizer Inc 5-HT receptor ligands and uses thereof
CA2469967A1 (fr) 2001-12-26 2003-07-10 Bayer Healthcare Ag Derives d'uree
US7790231B2 (en) 2003-07-10 2010-09-07 Brewer Science Inc. Automated process and apparatus for planarization of topographical surfaces
JP2008534542A (ja) * 2005-03-31 2008-08-28 ユセベ ファルマ ソシエテ アノニム オキサゾール部分又はチアゾール部分を含む化合物、それらの製造方法及びそれらの使用
JP2009530274A (ja) * 2006-03-15 2009-08-27 ワイス ヒスタミン−3アンタゴニストとしてのn−置換−アザシクリルアミン化合物
PE20081152A1 (es) * 2006-10-06 2008-08-10 Wyeth Corp Azaciclilaminas n-sustituidas como antagonistas de histamina-3
EP2170875A1 (fr) * 2007-07-16 2010-04-07 Wyeth LLC Dérivés d'aminoalkylazole en tant qu'antagonistes d'histamine-3

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070105834A1 (en) * 2004-05-25 2007-05-10 Sanofi-Aventis Tetrahydroisoquinoline sulfonamide derivatives, the preparation thereof, and the use of the same in therapeutics
US20080318952A1 (en) * 2007-05-18 2008-12-25 Keith John M Diaryl-substituted tetrahydroisoquinolines as histamine h3 receptor and serotonin transporter modulators

Also Published As

Publication number Publication date
IL216924A0 (en) 2012-03-01
MX2011012824A (es) 2012-01-27
RU2012102671A (ru) 2013-08-10
BRPI1011258A2 (pt) 2016-03-22
EP2445899B1 (fr) 2016-05-11
TW201103911A (en) 2011-02-01
UY32738A (es) 2011-01-31
SG176645A1 (en) 2012-01-30
AU2010264422A1 (en) 2012-02-02
NZ597219A (en) 2013-05-31
US8664245B2 (en) 2014-03-04
CN102803247A (zh) 2012-11-28
CO6480943A2 (es) 2012-07-16
PL2445899T3 (pl) 2017-08-31
PE20121403A1 (es) 2012-11-02
EP2445899A1 (fr) 2012-05-02
ZA201108838B (en) 2012-08-29
KR20120039555A (ko) 2012-04-25
CA2766154C (fr) 2015-04-07
ES2587064T3 (es) 2016-10-20
TN2011000620A1 (en) 2013-05-24
US20120149728A1 (en) 2012-06-14
MA33378B1 (fr) 2012-06-01
AU2010264422B2 (en) 2014-12-18
JP6053519B2 (ja) 2016-12-27
WO2010151611A1 (fr) 2010-12-29
JP2012531424A (ja) 2012-12-10
AR077223A1 (es) 2011-08-10
CN102803247B (zh) 2014-11-05
CA2766154A1 (fr) 2010-12-29
KR101804749B1 (ko) 2017-12-05
DOP2011000398A (es) 2012-01-31
RU2537847C2 (ru) 2015-01-10

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